Naringenin (NAR), 4′,5,7-trihydroxydihydroflavone, has a wide range of pharmacological activities but shows poor water solubility and low bioavailability. The pharmacokinetics and bioavailability of naringenin-nicotinamide cocrystal (NAR-NCT), which offers improved solubility, were evaluated in this study. Rats were orally administered NAR, a physical mixture of naringenin and nicotinamide (NAR + NCT), and NAR-NCT. The relative bioavailability of NAR-NCT was 175.09% of NAR, C_max was 8.43 and 2.06 times of NAR and NAR + NCT, respectively, Tmax was advanced from 0.49 h to 0.09 h, CL was decreased from 91.1 L/h/kg to 49.1 L/h/kg, and t_1/2 was increased from 5.37 h to 8.24 h, highlighting its rapid absorption and slow elimination. This study showed that NAR-NCT could improve the bioavailability of NAR.

中文翻译：

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LC-MS / MS对柚皮苷和柚皮苷-烟酰胺共晶体在大鼠体内的药代动力学比较。

柚皮素（NAR）4'，5,7-三羟基二氢黄酮具有广泛的药理活性，但水溶性差，生物利用度低。在这项研究中评估了提供改善的溶解度的柚皮苷-烟酰胺共晶体（NAR-NCT）的药代动力学和生物利用度。大鼠口服NAR，柚皮苷和烟酰胺的物理混合物（NAR + NCT）和NAR-NCT。NAR-NCT的相对生物利用度为NAR的175.09％，C _max分别为NAR和NAR + NCT的8.43和2.06倍，Tmax从0.49 h升高至0.09 h，CL从91.1 L / h / kg降低至49.1升/小时/千克，吨_1/2从5.37小时增加到8.24小时，突出了其快速吸收和缓慢消除的作用。这项研究表明，NAR-NCT可以提高NAR的生物利用度。